RS-33295-198：一种新型强效P-糖蛋白介导的多药耐药调节剂。
RS-33295-198: a novel, potent modulator of P-glycoprotein-mediated multidrug resistance.
作者信息
Slate D L, Bruno N A, Casey S M, Zutshi N, Garvin L J, Wu H, Pfister J R
机构信息
Institute of Biochemistry and Cell Biology, Palo Alto, CA, USA.
出版信息
Anticancer Res. 1995 May-Jun;15(3):811-4.
A novel multidrug resistance modulator, RS-33295-198, circumvented drug resistance in human, mouse, and Chinese hamster cell lines overexpressing P-glycoprotein. It enhanced the antiproliferative activity of doxorubicin, vincristine, etoposide, and paclitaxel and increased doxorubicin retention in multidrug-resistant hamster CHRC5 cells. RS-33295-198 modulated doxorubicin resistance in a murine P388/ADR leukemia model when administered ip via continuous minipump delivery, ip by bolus injection, and orally; it also improved the efficacy of vincristine toward P388/VCR leukemia when given ip or po. RS-33295-198 showed weak activity in enhancing doxorubicin efficacy against a multidrug-resistant human sarcoma xenograft.
一种新型多药耐药调节剂RS-33295-198可克服在过表达P-糖蛋白的人、小鼠和中国仓鼠细胞系中的耐药性。它增强了阿霉素、长春新碱、依托泊苷和紫杉醇的抗增殖活性，并增加了多药耐药仓鼠CHRC5细胞中阿霉素的滞留量。当通过连续微型泵腹腔内给药、腹腔推注给药和口服给药时，RS-33295-198在鼠P388/ADR白血病模型中调节阿霉素耐药性；当腹腔内或口服给药时，它也提高了长春新碱对P388/VCR白血病的疗效。RS-33295-198在增强阿霉素对多药耐药人肉瘤异种移植瘤的疗效方面表现出较弱的活性。
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